A Theoretical Investigation for Exploring the Potential Performance of Non-Fullerene Organic Solar Cells Through Side-Chain Engineering Having Diphenylamino Groups to Enhance Photovoltaic Properties.

The development of ecofriendly fabrication phenomenon is essential requirement for commercialization of non-fullerene acceptors. Recently, end-capped modeling is employed for computational design of five non-fullerene acceptors to elevate various photovoltaic properties. All new molecules are formulated by altering the peripheral acceptors of CH3-2F and DFT methodology is employed to explore the opto-electronic, morphological and charge transfer analysis. From the computational investigation, all reported molecules manifested red shifted absorption with remarkable reduced band gap. Among investigated molecules, FA1-FA3 evinced effectively decreased value of band gaps and designed molecules have low excitation energy justifying proficient charge transference. The lower values of binding energy of FA1 and FA2 suggest their facile exciton dissociation leading to improved charge mobility. By blending with J61 donor, FA4 have sufficiently enhanced value of VOC (1.72 eV) and fill factor (0.9228). Energy loss of the model (R) is 0.57 eV and statistical calculation demonstrate that all our modified molecules except FA3 has profoundly reduced energy loss compelling in its pivotal utilization. From accessible supportive outcomes of recent investigation, it is recommended that our modified chromophore exhibit remarkable noteworthy applications in solar cells for forthcoming innovations.

Formulation of Mentha piperita-Based Nanobiopesticides and Assessment of the Pesticidal and Antimicrobial Potential.

The excessive use of synthetic pesticides has detrimental impacts on humans, non-target organisms, and the environment. Insect pest management strategies are shifting toward biopesticides, which can provide a feasible and environmentally friendly green solution to the pest problem. The key objective of the present research work was the preparation of Mentha piperita-based nanobiopesticides with enhanced stability, solubility, and pesticidal potential. Nanobiopesticides based on the Mentha piperita extract were prepared using the antisolvent precipitation method. The central composite design of response surface methodology (RSM) was utilized to optimize different process parameters, e.g., the amounts of the stabilizer and plant extract. The nanosuspension of Mentha piperita prepared with the stabilizer SLS showed a particle size of 259 nm and a polydispersity index of 0.61. The formulated biopesticides in the form of nanosuspensions showed good antibacterial activities as compared to the Mentha piperita extract against two phytopathogenic bacterial strains, Clavibacter michiganensis and Pseudomonas syringae. The M. piperita nanosuspension had higher antifungal efficacy against A. niger and F. oxysporum than the Mentha piperita extract. The M. piperita extract and its nanosuspensions were tested for pesticidal activity against the stored-grain insects Tribolium castaneum and Sitophilus oryzae. Mentha piperita-based nanobiopesticides demonstrated significantly high (p < 0.05) average mortality of 84.4% and 77.7% against Tribolium castaneum and Sitophilus oryzae, respectively. Mentha piperita-based nanobiopesticides showed enhanced pesticidal potential and could be used as a good alternative to synthetic chemical pesticides.

Recent advances in synthesis and characterization of iron-nickel bimetallic nanoparticles and their applications as photo-catalyst and fuel additive.

Iron-nickel bimetallic nanoparticles (Fe-Ni BMNPs) are prepared by combining two different metals by using the bottom-up approach. The resulting material has entirely different properties as compared to both the metals. The product is examined by using different analytical instruments such as.; scanning electron microscope (SEM), transmission electron microscope (TEM), X-ray diffraction (XRD), MDIJADE, ORIGIN pro to characterize their morphology, crystallinity and elemental composition and the final data has been statistically analyzed. SEM findings show that most nanoparticles are irregular in form and range in size from 10 nm to 100 nm. The findings of the TEM verified that the particles between 10 nm and 50 nm are irregular in size shape. The products acquired utilized as a fuel additive to monitor oil effectiveness by studying various parameters. The degradation of methylene blue dye depends directly on the concentration of the nanocatalyst. Different parameters also use the freshly prepared bimetallic nanocatalyst to investigate the efficacy of the kerosene fuel. By adding a tiny quantity of the nanocatalyst, the value of the flash point and fire point is significantly reduced. The nanocatalyst does not affect the cloud point and pour point to a large extent. The bimetallic nanocatalyst therefore has very excellent catalytic characteristics.

Development of Nanosuspension of Artemisia absinthium Extract as Novel Drug Delivery System to Enhance Its Bioavailability and Hepatoprotective Potential.

A nanosuspension of Artemisia absinthium extract was formulated and characterized for the enhancement of bioavailability and better hepatoprotective efficacy. The nanosuspension of A. absinthium extract was formulated using an antisolvent precipitation technique, and various formulation parameters were optimized using response surface methodology (RSM). The optimized nanosuspension was characterized using AFM and FT-IR spectroscopy. The drug-release profile and oral bioavailability of the optimized nanosuspension were assessed with reference to coarse suspension. The DPPH radical scavenging method was used to measure the nanosuspension's antioxidant activity, and its in vivo hepatoprotective potential was assessed against CCl4-induced hepatic injury in rats. The developed optimized nanosuspension had suitable zeta potential of -11.9 mV, PDI of 0.285, and mean particle size of 253.8 nm. AFM study demonstrated a homogeneous population of nanoparticles with average size of 25 nm. The formulated nanosuspension of A. absinthium showed faster dissolution rate and 1.13-fold enhanced bioavailability as compared to the coarse suspension (plant extract). Furthermore, the nanoformulation had stronger antioxidant and hepatoprotective potential as compared to the unprocessed coarse extract. These results demonstrated that nanosuspension is a promising strategy for improving the oral bioavailability and bioactivities of A. absinthium extract.

Green inspired synthesis of zinc oxide nanoparticles using Silybum marianum (milk thistle) extract and evaluation of their potential pesticidal and phytopathogens activities.

Background: The green approaches for the synthesis of nanoparticles are gaining significant importance because of their high productivity, purity, low cost, biocompatibility, and environmental friendliness. Methods: The aim of the current study is the green synthesis of zinc oxide nanoparticles (ZnO-NPs) using seed extracts of Silybum marianum, which acts as a reducing and stabilizing agent. central composite design (CCD) of response surface methodology (RSM) optimized synthesis parameters (temperature, pH, reaction time, plant extract, and salt concentration) for controlled size, stability, and maximum yields of ZnO-NPs. Green synthesized ZnO-NPs was characterized using UV-visible spectroscopy and Zetasizer analyses. Results: The Zetasizer confirmed that green synthesized ZnO-NPs were 51.80 nm in size and monodispersed in nature. The UV-visible results revealed a large band gap energy in the visible region at 360.5 nm wavelength. The bioactivities of green synthesized ZnO-NPs, including antifungal, antibacterial, and pesticidal, were also evaluated. Data analysis confirmed that these activities were concentration dependent. Bio-synthesized ZnO-NPs showed higher mortality towards Tribolium castaneum of about 78 ± 0.57% after 72 h observation as compared to Sitophilus oryzae, which only displayed 74 ± 0.57% at the same concentration and time intervals. Plant-mediated ZnO-NPs also showed high potential against pathogenic gram-positive bacteria (Clavibacter michiganensis), gram-negative bacteria (Pseudomonas syringae), and two fungal strains such as Fusarium oxysporum, and Aspergillums niger with inhibition zones of 18 ± 0.4, 25 ± 0.4, 21 ± 0.57, and 19 ± 0.4 mm, respectively. Conclusion: The results of this study showed that Silybum marianum-based ZnO-NPs are cost-effective and efficient against crop pests.

Investigation of phytotherapeutic potential of herbal mixtures and their effects on salbutamol induced cardiotoxicity and hyperlipidemia in rabbits.

BACKGROUND: Cardiovascular diseases (CVDs) are the major cause of deaths all over the world. The high level of blood cholesterol and oxidative stress are major risk factors for heart diseases. The phytotherapeutics have attracted attention as potential agents for preventing and treating oxidative stress associated diseases. The objective of present study was to evaluate the synergetic cardio-protective and antilipidemic potential of medicinal plants viz. Coriandrum sativum, Piper nigrum and Cactus grandiflorus. Cardio-protective and anti-lipidemic potential of herbal mixture was evaluated against salbutamol induced cardiotoxicity in rabbits. For this purpose, rabbits were divided into six groups as normal control, salbutamol control, curative and standard drug curative. RESULTS: Salbutamol significantly (p < 0.05) increased the level of serum cardiac biomarkers (ALT, CK-MB, AST and LDH) and lipids (LDL, triglycerides, cholesterol) in rabbits. The prior and post administration of herbal mixture significantly (p < 0.05) lowered the elevated level of serum cardiac biomarkers and lipids equal to normal control. Gross pathological examination revealed that heart of salbutamol control animals became hardened, congested and were enlarged than preventive and curative groups. The phytotherapeutic analysis of medicinal plants revealed the presence of phenols, tannins, alkaloids and steroids. CONCLUSION: The results showed that this herbal mixture has strong cardio-protective and anti-lipidemic potential.

Formulation and Process Optimization of Rauvolfia serpentina Nanosuspension by HPMC and In Vitro Evaluation of ACE Inhibitory Potential.

Angiotensin converting enzyme (ACE) overactivation is one of the primary causes of hypertension, which leads to cardiovascular disorders all over the world. In the scientific world, nanosuspension is a novel area of study that could offer an alternative treatment for active pharmaceuticals that are not well soluble in water. Since active compounds' bioavailability is reduced by their poor solubility, there are eventually fewer applications. Drug solubility, dissolving rate, and bioavailability are improved by nanosuspension, which shrinks medication particle size into the nanoscale range and boosts the surface area to volume ratio of the drug. There is a need to prepare Rauvolfia serpentina's nanosuspension in order to get around some of the major challenges that it faces because of its poor solubility and wide range of biological activities. Using the antisolvent precipitation approach, a nanosuspension of Rauvolfia serpentina was created with hydroxy propyl methyl cellulose (HPMC). Rouvolfia serpentina nanosuspensions were prepared using a design of expert (DOE) approach, which allowed for the evaluation of key process parameters. To get an optimal sample, the effects of stabilizer concentration and anti-solvent volume on particle size, zeta potential, and PdI using CCD-RSM were investigated. Using the substrate Hippuryl-histidyl-leucine, the in vitro ACE inhibitory potential was assessed. On human erythrocytes, the safety of nanosuspension was evaluated in vitro. The ideal value of independent variables was discovered to be 0.25% w/v in order to achieve the desired response. Using scanning electron microscopy, the morphology of optimized nanosuspension was discovered to be rod-shaped (SEM). Compared to nanoformulation, crude extract had higher ACE inhibitory potential (83.11%). Human erythrocytes were found to be unaffected by nano-sized particles.

Formulation and characterisation of Azadirachta indica nanobiopesticides for ecofriendly control of wheat pest Tribolium castaneum and Rhyzopertha dominica.

This study aimed to formulate the green, sustainable, and ecofriendly nanobiopesticides of Azadirachta indica with enhanced pest control efficacy. Nanoprecipitation method was used for the development of nanobiopesticides. Optimisation was done by response surface methodology. Nanoformulations were characterised by zetasizer, scanning electron microscopy, energy dispersive x-ray spectroscopy, atomic force microscopy, and Fourier transform infrared spectroscopy. Pesticidal potential of nanosuspensions was evaluated by insecticide impregnated filter paper method. Optimised nanobiopesticide showed an average particle size of 275.8 ± 0.95 nm, polydispersity index (PDI) 0.351 ± 0.002, and zeta potential of -33 ± 0.90 mV. Nanobiopesticides exhibited significantly higher mortality rates of 86.81 ± 3.04 and 84.97 ± 2.83% against Tribolium castaneum and Ryzopertha dominica, respectively, as compared to their crude extract. Minor change in particle size from 275.8 ± 0.95 to 298.8 ± 1.00 nm and PDI from 0.351 ± 0.002 to 0.445 ± 0.02 were observed after 3 months of storage at 4 °C. Pesticidal efficacy of A. indica was significantly enhanced by the formulation of its nanobiopesticides.

Green synthesized silver nanoparticles: Optimization, characterization, antimicrobial activity, and cytotoxicity study by hemolysis assay.

Green nanotechnology has emerged as a viable option for the production of nanoparticles. The purpose of the current investigation was to synthesize silver nanoparticles (AgNPs) using Eucalyptus camaldulensis and Terminalia arjuna extracts, as well as their combinations, as green reducing and capping agents. The parameters (concentration of silver nitrate solution and plant extract, time, pH, and temperature) were optimized for maximal yields, regulated size, and stability of silver nanoparticles. The ultraviolet-visible spectrophotometer (UV-Vis) and the surface plasmon resonance band (SPR) were used to validate the synthesis of AgNPs. The size, shape, and stability of nanoparticles were assessed using a zeta analyzer and a scanning electron microscope (SEM). The biomolecules responsible for the reduction of silver ion (Ag+) and the stability of silver nanoparticles generated with the plant extracts were identified using Fourier-transform infrared spectroscopy (FTIR). The agar-well diffusion method was used to test the antimicrobial activity of biosynthesized nanoparticles against Bacillus subtilis, Staphylococcus aureus, Pasteurella multocida, and Escherichia coli. When 1 mM of silver nitrate (AgNO3) was added to plant extracts and incubated for 60 min at 75°C in a neutral medium, maximum nanoparticles were produced. Biosynthesized silver nanoparticles were stable, spherical, and monodispersed according to zeta potential and scanning electron microscopy. Silver nanoparticles synthesized with combination 2 and T. arjuna showed the highest zone of inhibition (16 mm) against B. subtilis while combination 3 showed the largest zone of inhibition against S. aureus (17 ± 0.8). It was concluded that greenly produced silver nanoparticles showed good antibacterial activity while causing negligible cytotoxicity.

Isolation and characterization of novel antihypertensive bioactive peptides from brassica napus and angiotensin-converting enzyme (ace) inhibition potential.

Present study aimed to explore the antihypertensive potential of bioactive peptides isolated from Brassica napus protein as inhibitor of angiotensin converting enzyme. Protein was extracted and assessed for antihypertensive potential. The extracted protein showed 72% antihypertensive activity/potential with IC50 value of 24±5.60µg/mL. Thirty-one fractions of peptides were isolated by hydrolyzing protein at different time intervals, pH, temperature and enzyme/substrate ratio. The antihypertensive potential of all isolated fractions was measured. It was found that only one peptide fraction exhibited significantly high (75%) antihypertensive potential. This hydrolyzed fraction was characterized through Liquid-Chromatography-Electrospray-Ionization-Mass-Spectrometry (LC-ESI-MS/MS). Eleven bioactive peptides were identified in hydrolyzate of Brassica napus which include Serine-Threonine, Methionine-Valine, Methionine-Leucine, Glutamine-Phenylalanine, Alanine-Threonine-Phenylalanine, Alanine-Leucine-Proline-Glycine, Valine-Alanine-Phenylalanine-Glycine, Aspartic acid-Proline-Methionine-Glutamine, Valine-Glutamine-Cysteine-Tyrosine, Methionine-Cysteine-Tyrosine-Tyrosine-Phenylalanine and Alanine-Leucine-Leucine-Alanine-Cysteine-Proline-Alanine. The current study showed that Brassica napus is an important food, having high amount of bioactive peptides with high antihypertensive potential, can control blood pressure very efficiently.

Biologically Synthesized Peptides Show Remarkable Inhibition Activity against Angiotensin-Converting Enzyme: A Promising Approach for Peptide Development against Autoimmune Diseases.

Angiotensin-converting enzyme (ACE) regulates several biological functions besides its vital role in immune functions. ACE is elevated in immune cells in inflammatory diseases including atherosclerosis, granuloma, chronic kidney disease, and also autoimmune diseases, like multiple sclerosis, rheumatoid arthritis, and type I diabetes. No significant information prevails in the literature regarding the isolation, identification, and profiling of potential ACE inhibitory peptides. In the present study, indigenous crop varieties like seeds (peanut, corn, oat, sunflower, chickpea, parsley, cottonseed, papaya, sesame, and flaxseed) were used to evaluate their ACE inhibition activity. Variables including hydrolysis time, enzyme-to-substrate ratio (E/S), pH, and temperature were standardized to acquire the most suitable and optimum ACE inhibition activity. Seeds of cotton, chickpea, and peanuts displayed remarkably maximum ACE inhibition activity than other plants. The study disclosed that maximum ACE inhibitory activity (86%) was evaluated from cottonseed at pH 8.0, temperature of 45°C, hydrolysis time of 2 hrs, and enzyme to the substrate (E/S) ratio of 1 : 5 followed by peanuts (76%) and chickpea (55%). SDS-PAGE confirmed that vicilin protein is present in cottonseed and peanut seed while cruciferin and napin proteins are present in chickpeas. LC-MS/MS analysis disclosed potential novel peptides in hydrolyzed cottonseed that can be ascribed as potential ACE inhibitors which have never been reported and studied earlier. The current study further showed that cottonseed peptides due to their promising ACE inhibitory activity can be a valuable source in the field of ACE inhibitor development.

Evaluation and optimization of nanosuspensions of Chrysanthemum coronarium and Azadirachta indica using Response Surface Methodology for pest management.

The rapidly emerging field of nanotechnology is considered an important achievement in the agriculture sector to increase the pest mortality rate and improve the crop production. The present study evaluates the novel pesticidal and anti-microbial activities of Chrysanthemum coronarium and Azadirachta indica in the nano-suspensions form. The anti-solvent precipitation method was used to formulate nano-suspensions proposed by Response Surface Methodology (RSM). Physicochemical nature of plant extracts and nano-suspensions was characterized through analysis of Zeta-sizer, FT-IR, and HPLC. Characterization results revealed a minimum particle size of 121.1 and 170.1 nm for Chrysanthemum coronarium and Azadirachta indica, respectively. The pesticidal activity of nano-suspension was performed against red flour beetle (RFB) and lesser grain borer (LGB) pests, which showed the maximum mortality rate of 100% with 100% concentration of plant extracts and nano-suspensions of Chrysanthemum coronarium and Azadirachta indica against both insects. In comparison, the combination of these both plant extracts revealed the maximum 100% mortality with a 50% concentration of nano-suspensions (mixing ratio 1:1) after 72 h. The antibacterial activity showed the maximum zone inhibition of 9.96 ± 0.17 and 14.17 ± 0.50 mm against S.aureus and E. coli with nano-suspension of Chrysanthemum coronarium, and 12.09 ± 0.11 and 14.10 ± 0.49 mm with nano-suspension of Azadirachta indica, respectively. It is concluded that individual nano-suspensions showed better pesticidal as well as antimicrobial activities than combinations. However, the constructed nanosuspension can be applied to control the plant pests and diseases simultaneously.

Isolation and characterization of antihypertensive peptides from soy bean protein

Proteins and peptides are the most diverse biomolecules found in nature and make our interest due to their wide applications in food and pharmaceutical industry. Angiotensin Converting Enzyme (ACE) plays a major role in controlling blood pressure. The inhibition of ACE with peptides is a main target in the regulation of hypertension. The objective of the present study was to investigate the therapeutic potential of soy bean. This was accomplished by isolation of ACE inhibitory peptides using response surface methodology (RSM) and characterization of these bioactive peptides by mass spectrometry. 31 hydrolyzed fractions were isolated and evaluated for their ACE inhibition potential. Hydrolyzed fraction having highest ACE inhibitory activity was characterized by liquid chromatography-mass spectrometry (LC-MS) technique. RSM results showed maximum ACE inhibition potential (64%) by hydrolyzate was obtained at 45 ºC temperature, pH 8.0, E/S 0.2 in 2 hours hydrolysis time. Results of LC-MS analysis revealed Ser-Gly, Ser-Pro, Met-Ala, His-Ala, Lys-Pro, Phe-Thr, Met-Leu, Pro-Arg, Ala-Pro-Val, Pro-Ala-Leu, Val-Met-Gly, Pro-Leu-Val, Pro-Pro-Gln, His-Arg-Gly, Ser-Phe-Val-Leu, Ala-Val-His-Try, Arg-Thr-Val-Arg, His-His-Tyr-Leu-Val, Asp-Gly-Ala-Cys-Ser-Ala-Asn and MetVal-Thr-Gly-Pro-Gly-Cys-His bioactive peptides in hydrolyzed fraction of soy bean. Our data provide evidence that response surface methodology is a good approach for isolation of antihypertensive bioactive peptides with more potent activity as nutraceuticals or pharmaceuticals. Therefore soy bean can be use for industrial production of pharmaceutical grade natural medicines for handling high blood pressure.

The broad-spectrum antiviral recommendations for drug discovery against COVID-19.

Despite to outbreaks of highly pathogenic beta and alpha coronaviruses including severe acute respiratory syndrome coronavirus (SARS-CoV), Middle East respiratory syndrome coronavirus (MERS-CoV), and human coronavirus, the newly emerged 2019 coronavirus (COVID-19) is considered as a lethal zoonotic virus due to its deadly respiratory syndrome and high mortality rate among the human. Globally, more than 3,517,345 cases have been confirmed with 243,401 deaths due to Acute Respiratory Distress Syndrome (ARDS) caused by COVID-19. The antiviral drug discovery activity is required to control the persistence of COVID-19 circulation and the potential of the future emergence of coronavirus. However, the present review aims to highlight the important antiviral approaches, including interferons, ribavirin, mycophenolic acids, ritonavir, lopinavir, inhibitors, and monoclonal antibodies (mAbs) to provoke the nonstructural proteins and deactivate the structural and essential host elements of the virus to control and treat the infection of COVID-19 by inhibiting the viral entry, viral RNA replication and suppressing the viral protein expression. Moreover, the present review investigates the epidemiology, diagnosis, structure, and replication of COVID-19 for better understanding. It is recommended that these proteases, inhibitors, and antibodies could be a good therapeutic option in drug discovery to control the newly emerged coronavirus.HighlightsCOVID-19 has more than 79.5% identical sequence to SARS-CoV and a 96% identical sequence of the whole genome of bat coronaviruses.Acute respiratory distress syndrome (ARDS), renal failure, and septic shock are the possible clinical symptoms associated with COVID-19.Different antivirals, including interferons, ribavirin, lopinavir, and monoclonal antibodies (mAbs) could be the potent therapeutic agents against COVID-19.The initial clinical trials on hydroquinone in combination with azithromycin showed an admirable result in the reduction of COVID-19.The overexpression of inflammation response, cytokine dysregulation, and induction of apoptosis could be an well-organized factors to reduce the pathogenicity of COVID-19.

Synthesis and biological evaluation of Ellettaria cardamomum (Cardamom) Phytosomes.

Ellettaria cardamomum (Cardamom) is an excellent antioxidant and its phytochemicals possess astounding detox properties. The bioactives of E. cardamomum have low bioavailability due to complex molecular structure. The main aim of this research was to formulate the E. cardamomum loaded phytosomes to improve the bioavailability with better ACE inhibition potential. The phytosomes were prepared by thin layer hydration technique. Various synthetic parameters for formulation of phytosomes were optimized by response surface methodology. Formulated phytosomes were characterized through spectroscopically and their biological activities eg. ACE inhibition were also investigated. Resultantly, the optimal production of phytosomes was achieved with the equal quantity (300 mg) of E. cardamomum and phospholipids at the time of 20 minutes of hydration. UV-Visible spectra confirmed the chemical and physical interaction between phospholipid and bioactives functional groups. The optimized E. cardamomum phytosome had 71% of entrapment efficiency. The average vesicle size of phytosomes was 577.8 nm with polydispersity index 0.443. SEM analysis revealed that phytosomes were spherical in shape. The phytosomes of E. cardamomum showed higher antioxidant and antimicrobial activities than its crude extract. The ACE inhibition activity of phytosomes (46%) was enhanced than the crude extract (39 %).

The Role of Polyphenol (Flavonoids) Compounds in the Treatment of Cancer Cells.

Cancer remains a second leading cause of deaths and major public health problem. It occurs due to extensive DNA damage caused by ultraviolet radiations, ionizing radiations, environmental agents, therapeutic agents, etc. Among all cancers, the most frequently diagnosed cancers are lung (12.7%), breast (10.9%), colorectal (9.7%), and gastric cancer (7.81%). Natural compounds are most favorable against cancer on the count of their anti-cancerous ability, easy to avail and efficient. Among natural compounds, polyphenols (flavonoids, catechin, hesperetin, flavones, quercetin, phenolic acids, ellagic acid, lignans, stilbenes, etc.) represent a large and diverse group used in the prevention and treatment of cancer. Natural flavonoids are derived from different plant sources and from various medicinal plants including Petroselinum crispum, Apium graveolens, Flemingia vestita, Phyllanthus emblica, etc. Natural flavonoids possess antioxidant, anti-inflammation, as well as anti-cancerous activities through multiple pathways, they induce apoptosis in breast, colorectal, and prostate cancers, lower the nucleoside diphosphate kinase-B activity in lung, bladder and colon cancers, inhibit cell-proliferation and cell cycle arrest by suppressing the NF-kB pathway in various cancers, etc. The current review summarized the anticancer activities of natural polyphenols and their mechanisms of action.

Nanosuspension enhances dissolution rate and oral bioavailability of Terminalia arjuna bark extract in vivo and in vitro

Objective: To enhance the dissolution rate and oral bioavailability of Terminalia arjuna bark extract by formulating its nanosuspension. Methods: Nanoprecipitation approach was used for the formulation of nanosuspension using polysorbate-80 as a stabilizer. The formulated nanosuspension was assessed for particle size, polydispersity index, zeta potential value and for in vitro dissolution study. Oral bioavailability studies were carried out in Wistar male albino rats by administering a single dose (50 mg/kg. b. wt) of the formulated nanosuspension and coarse suspension. The storage stability of the formulated nanosuspension was determined after three months of storage at room temperature and under the refrigerated condition. Mutagenicity assay was carried out to evaluate the toxicity of the formulated nanosuspension using two mutant strains (Salmonella typhimurium TA100 and Salmonella typhimurium TA98).Results: The mean particle size of the formulated nanosuspension was 90.53 nm with polydispersity index and zeta potential values of 0.175 and ?15.7 mV, respectively. Terminalia arjuna nanosuspension showed improved dissolution rate and 1.33-fold higher oral bioavailability than its coarse suspension. The formulated nanosuspension also showed better stability under the refrigerated condition and was non-mutagenic against both strains. Conclusions: Our study demonstrates that nanosuspension technology can effectively enhance the dissolution rate and oral bioavailability of Terminalia arjuna bark extract.

Increased Oral Bioavailability of Piperine from an Optimized Piper nigrum Nanosuspension.

The aim of the present study was to enhance the pharmaceutical potential and oral bioavailability of piperine, which is the bioactive constituent of Piper nigrum, using the nanosuspension approach. Nanoprecipitation, which is a simple and reproducible process, was used for nanosuspension formulation. To prepare a pharmaceutical-grade nanosuspension with the required particle size, important formulation parameters (amount of plant extract, concentration of stabilizer, and antisolvent-to-solvent ratio) were optimized using the central composite design of response surface methodology. The optimized nanosuspension was characterized using scanning electron microscopy, atomic force microscopy, Fourier transform infrared spectroscopy, and in vitro dissolution testing as well as by measuring the zeta potential. In vivo pharmacokinetic studies were conducted to determine the bioavailability of the prepared nanosuspension. Results of the optimization study indicated that 0.13% plant extract, 0.25% stabilizer, and an antisolvent-to-solvent ratio of 10.0 were the best parameters to obtain a homogeneous nanosuspension with the required particle size. The optimized nanosuspension demonstrated a mean particle size, polydispersity index, and zeta potential of 172.5 nm, 0.241, and - 16.6 mV, respectively. The results of the characterization studies illustrated that the nanosuspension was in the nanometer size range and had good surface morphology. The optimized nanosuspension showed a better dissolution rate and a 3.65-fold higher oral bioavailability for the P. nigrum nanosuspension than its coarse suspension. The present outcomes clearly demonstrated that to obtain an effective therapeutic potential, nanoformulation of medicinal plants is a better alternative than conventional dosage forms.

Identification of Hypotensive Biofunctional Compounds of Coriandrum sativum and Evaluation of Their Angiotensin-Converting Enzyme (ACE) Inhibition Potential.

The aim of this study was to identify and characterize the bioactive compounds of Coriandrum sativum responsible for the treatment of hypertension and to explore their mechanism of action as angiotensin-converting enzyme (ACE) inhibitors. Bioactive fractions like alkaloids, flavonoids, steroids, and tannins were extracted and evaluated for their ACE inhibition potential. Among them, only flavonoid-rich fraction showed high ACE inhibition potential with IC50 value of 28.91 ± 13.42 µg/mL. The flavonoids were characterized through LC-ESI-MS/MS. Seventeen flavonoids were identified in this fraction of Coriandrum sativum in negative ionization mode which includes pinocembrin, apigenin, pseudobaptigenin, galangin-5-methyl ether, quercetin, baicalein trimethyl ether, kaempferol dimethyl ether, pinobanksin-5-methylether-3-O-acetate, pinobanksin-3-O-pentenoate, pinobanksin-3-O-phenylpropionate, pinobanksin-3-O-pentanoate, apigenin-7-O-glucuronoide, quercetin-3-O-glucoside, apigenin-3-O-rutinoside, rutin, isorhamnetin-3-O-rutinoside, and quercetin dimethyl ether-3-O-rutinoside, while six flavonoids including daidzein, luteolin, pectolinarigenin, apigenin-C-glucoside, kaempferol-3-7-dimethyl ether-3-O-glucoside, and apigenin-7-O-(6-methyl-beta-D-glucoside) were identified in positive ionization mode. The results of this study revealed that Coriandrum sativum is a valuable functional food that possesses a number of therapeutic flavonoids with ACE inhibition potential that can manage blood pressure very efficiently.

Cardioprotective and Metabolomic Profiling of Selected Medicinal Plants against Oxidative Stress.

In this research work, the antioxidant and metabolomic profiling of seven selected medicinally important herbs including Rauvolfia serpentina, Terminalia arjuna, Coriandrum sativum, Elettaria cardamom, Piper nigrum, Allium sativum, and Crataegus oxyacantha was performed. The in vivo cardioprotective potential of these medicinal plants was evaluated against surgically induced oxidative stress through left anterior descending coronary artery ligation (LADCA) in dogs. The antioxidant profiling of these plants was done through DPPH and DNA protection assay. The C. oxyacantha and T. arjuna showed maximum antioxidant potential, while the E. cardamom showed poor antioxidative strength even at its high concentration. Different concentrations of extracts of the said plants exhibited the protection of plasmid DNA against H2O2 damage as compared to the plasmid DNA merely treated with H2O2. The metabolomic profiling through LC-MS analysis of these antioxidants revealed the presence of active secondary metabolites responsible for their antioxidant potential. During in vivo analysis, blood samples of all treatment groups were drawn at different time intervals to analyze the cardiac and hemodynamic parameters. The results depicted that the group pretreated with HC4 significantly sustained the level of CK-MB, SGOT, and LDH as well as hemodynamic parameters near to normal. The histopathological examination also confirmed the cardioprotective potential of HC4. Thus, the HC4 being safe and inexpensive cardioprotective herbal combination could be considered as an alternate of synthetic drugs.